Solian, 100 mg/ml 60 ml

Amisulpride has a high selective affinity for dopaminergic receptors of subtypes D 2 /D 3 and no affinity for subtypes D 1, D 4 and D 5.

In contrast to classical and atypical neuroleptics, amisulpride has no affinity for serotonin receptors, histamine H1 -receptors, ?-adrenoreceptors and choline receptors.

When used in high doses it blocks postsynaptic D 2 -receptors localized in limbic structures unlike analogous receptors in striatum. It does not cause catalepsy and does not lead to development of hypersensitivity of dopamine D 2 -receptors after repeated treatment.

At low doses, it predominantly blocks presynaptic D 2 /D 3 -receptors, stimulating dopamine release.
Its atypical pharmacological profile accounts for the antipsychotic effect of amisulpride at high doses resulting from blockade of postsynaptic dopamine receptors and its effectiveness at low doses on negative symptoms resulting from blockade of presynaptic dopamine receptors.

Amisulpride is less likely to cause extrapyramidal side effects, which may be due to its predominant limbic activity.

In patients with schizophrenia with acute seizures, Solian acts on both secondary negative symptoms and affective symptoms (including depressed mood and retardation).

Indications

Acute and chronic schizophrenia accompanied by pronounced productive (including delusions, hallucinations, thought disorders) and/or negative (including affective flatness, lack of emotionality and withdrawal from communication) disorders, including in patients with predominantly negative symptomatology.

Active ingredient

Composition

1 ml contains:

amisulpride 100 mg

How to take, the dosage

In acute psychotic episodes, the recommended dose is 400 to 800 mg/day. In individual cases, if necessary, the dose may be increased to 1200 mg/day. Doses are increased taking into account individual tolerability of the drug. The maximum daily dose should not exceed 1200 mg.

In mixed negative and productive symptoms, doses should be tailored to provide optimal control of productive symptoms: average of 400 mg to 800 mg/day Maintenance treatment should be set individually at the minimum effective doses.

The recommended daily dose ranges from 50 to 300 mg. Dose selection should be individualized.

In elderly patients, Solian should be prescribed with extreme caution because of the possible development of arterial hypotension or excessive sedation.

In doses greater than 400 mg/day, Solian should be prescribed in 2 doses.

Interaction

Combinations that are contraindicated: With dopaminergic agonists (including amantadine, apomorphine, bromocriptine, cabergoline, entacapone, lisuride, pergolide, pyribedil, pramipexole, quinagolide, ropinirole, selegiline), except in patients with Parkinson’s disease. Dopaminergic agonists and neuroleptics show mutual antagonism. In extrapyramidal syndrome caused by neuroleptics, anticholinergic drugs should be used instead of dopaminergic agonists. Concomitant use of Solian with sultopride increases the risk of ventricular arrhythmias, especially atrial fibrillation.

Combinations not recommended: With drugs that may cause pirouette-type arrhythmias: Class Ia (including quinidine, hydroquinidine, disopyramide ) and Class III (including amiodarone, sotalol, dofetilide, ibutilide) antiarrhythmic drugs, some neuroleptics (including Thioridazine, chlorpromazine, levomepromazine, trifluoperazine, cyamemazine, sulpiride, thiapride, pimozide, haloperidol, droperidol ) and other drugs (incl. Bepridil, cisapride, difemanil, IV erythromycin, misolastin, IV vincamine, halofantrine, sparfloxacin, gatifloxacin, moxifloxacin, pentamidine, IV spiramycin). The risk of ventricular arrhythmias, especially the development of pirouette arrhythmias, increases. If a combination of drugs cannot be avoided, QT interval control and ECG monitoring should be initiated before prescribing. Ethanol enhances the sedative effects of neuroleptics. Alcohol consumption and use of drugs containing alcohol should be avoided. Mutual antagonism between levodopa and neuroleptics should be considered when prescribing these drugs. In patients with Parkinson’s disease, the use of minimal effective doses of both drugs is recommended.

Combinations requiring special caution: With drugs that cause bradycardia (including Beta-adrenoblockers (except sotalol/ calcium channel blockers that cause bradycardia – diltiazem and verapamil), clonidine, guanfacine, foxglove drugs, cholinesterase inhibitors (including donepezil, rivastigmine, tacrine, ambenonium, galantamine, pyridostigmine, neostigmine). With drugs that may cause hypokalemia (including potassium withdrawing diuretics, laxatives, IV amphotericin B, glucocorticoids, tetracosactides). With the above drug combinations, the risk of ventricular arrhythmias, especially the development of pirouette-type arrhythmias, remains.

Combinations to be taken into account: With antihypertensive agents and beta-blockers in heart failure (including bisoprolol, carvedilol, metoprolol) has a vasodilator effect, increasing the risk of orthostatic hypotension (additive effect). With morphine derivatives (including analgesics, cough medicines), barbiturates, benzodiazepines and other anxiolytics, hypnotics, sedative antidepressants (including amitriptyline, doxepin, mianserine, mirtazapine, trimipramine), sedative antihistamines, central antihypertensive agents, neuroleptics and other medicines (including baclofen, taclofen and other drugs).baclofen, thalidomide, pizotifen ) lead to a pronounced increase in CNS depression (reduced concentration and danger to drivers and machine operators).

Special Instructions

The development of malignant neuroleptic syndrome characterized by hyperthermia, muscle rigidity, peripheral nervous system dysfunction, elevated CPK levels is possible. If hyperthermia develops, especially with high-dose use, all antipsychotic drugs (including Solian) should be discontinued.

As amisulpride is excreted by the kidneys, the drug dose and therapy regimen should be adjusted if renal function is severely impaired. There is no experience of this medicine use in patients with severe renal dysfunction (CKG less than 10 ml/min).

As the drug is poorly metabolized, no dose reduction is required in patients with impaired hepatic function.

Due to the possible lowering of the seizure threshold when using amisulpride, patients with a history of epilepsy require continuous monitoring during therapy with Solian.

In elderly patients, amisulpride should be used with special caution because of the possible risk of arterial hypotension or excessive sedation.

In Parkinson’s disease, caution should be exercised when prescribing antidopaminergic drugs and amisulpride because of the possible worsening of the condition. Amisulpride should be used only if neuroleptic therapy cannot be avoided.

Amisulpride causes dose-dependent prolongation of the QT interval, thereby increasing the risk of serious ventricular arrhythmias (pirouette type). Before prescribing the drug, and, if possible, depending on the clinical condition of the patient, it is recommended to control the factors contributing to arrhythmias: bradycardia (heart rate less than 55 bpm), hypokalemia, congenital prolongation of the QT interval.

In patients who require long-term treatment with neuroleptics, an ECG should be performed during the initial status evaluation.

Due to the lactose content of the tablets, the drug is contraindicated in congenital galactosemia, glucose or galactose malabsorption syndrome or lactase deficiency.

Impact on ability to drive and operate machinery: Amisulpride affects reaction speed, which may impair the ability to engage in potentially dangerous activities.

Contraindications

– Concomitant prolactin-dependent tumors (including prolactinoma of the pituitary gland, breast cancer).
– Pheochromocytoma.
– Severe renal insufficiency (CK less than 10 ml/min).
– Combined use with sultopride.
– Combined use with dopaminergic agonists (including amantadine, apomorphine, bromocriptine, cabergoline, entacapone, lisuride, pergolide, pyribedil, pramipexole, quinagolide, ropinirole, selegiline ) except in patients with Parkinson’s disease.
– Children under 14 years old.
– Lactation period (breast-feeding).
– Hypersensitivity to amisulpride and other components of the preparation.

The drug should be used with caution in:
– Pregnancy.
– Epilepsy.
– Parkinsonism.
– Renal failure.
– In elderly patients.

Side effects

CNS disorders: Often – insomnia, anxiety, agitation; sometimes – extrapyramidal symptoms (including tremor, hypertension, hypersalivation, akathisia, hypokinesia), the intensity of which at maintenance doses is usually moderate; symptoms are partially reversible without withdrawal of Solian with anticholinergic antiparkinsonian agents (incidence of dose-dependent extrapyramidal symptoms remains very low when treating patients with predominantly negative symptoms with doses of 50-300 mg/day); rarely – daytime sleepiness; very rarely – acute dystonia (including spastic torticollis, torsadesades de pointes, torsades de pointes).including spastic torticollis, oculogyric crises, trismus), which is reversible and corrected with antiparkinsonian agents; with long-term use – tardive dyskinesia, characterized by rhythmic, involuntary movements mainly of tongue and/or face (antiparkinsonian agents are ineffective and may cause worsening of symptoms); in single cases – malignant neuroleptic syndrome, convulsive seizures.

Digestive system disorders: Rarely – constipation, nausea, vomiting, dry mouth; in isolated cases – increased activity of liver enzymes (mainly transaminases).

Endocrine system disorders: Often – increased plasma prolactin levels (reversible after drug withdrawal) which may cause galactorrhea, amenorrhea, gynecomastia, breast swelling, impotence, frigidity as well as weight gain.

Cardiovascular system disorders: Rarely – arterial hypotension, bradycardia, prolongation of QT interval; very rarely – atrial fibrillation.

Others: In some cases – allergic reactions.

Overdose

There is limited experience with amisulpride overdose.

Symptoms: aggravation of known pharmacological effects of the drug (including drowsiness, sedation, arterial hypotension, extrapyramidal symptoms, coma ).

Treatment: in acute overdose the possible combination with other drugs should be studied and necessary measures should be taken: close control of vital body functions; ECG monitoring (risk of QT interval prolongation); in case of serious extrapyramidal symptoms, anticholinergic agents should be prescribed. Hemodialysis is ineffective. There is no specific antidote for amisulpride.

Pregnancy use

The safety of amisulpride use in pregnancy has not been established.

Hence, use of the drug in pregnancy is not recommended unless the anticipated benefit to the mother justifies the potential risk to the fetus.

The use of amisulpride during lactation is contraindicated.